Imunofar (Ciclosporin)

• Ciclosporin is used to modulate immune activity in several disease categories.
• Organ transplantation: prevents acute and chronic graft rejection by inhibiting calcineurin‑dependent T‑lymphocyte activation, thereby reducing interleukin‑2 production and immune‑mediated damage to the transplanted organ.
• Rheumatoid arthritis: diminishes synovial inflammation and joint damage in patients with moderate to severe disease, especially when conventional disease‑modifying antirheumatic drugs are insufficient or not tolerated.
• Psoriasis: controls severe plaque psoriasis by suppressing the overactive immune response in the skin, leading to reduced scaling, erythema, and plaque formation.

• Ciclosporin binds to the intracellular protein cyclophilin, forming a complex that inhibits the phosphatase activity of calcineurin. This blockade prevents dephosphorylation of nuclear factor of activated T‑cells (NF‑AT), a transcription factor required for interleukin‑2 gene expression. Consequently, T‑lymphocyte activation and proliferation are reduced, leading to broad immunosuppression. The effect is dose‑dependent and reversible upon discontinuation, allowing modulation of immune responses without complete ablation of host defense mechanisms.

Ciclosporin may be associated with a range of adverse reactions, varying from mild to serious.

Common Side Effects

• Headache: mild to moderate intensity, often transient.
• Tremor: fine shaking of hands or limbs.
• Hypertension: elevated blood pressure requiring monitoring.
• Hyperlipidemia: increased cholesterol or triglyceride levels.

Serious or Rare Side Effects

• Nephrotoxicity: impaired kidney function that may be irreversible.
• Infections: heightened susceptibility to bacterial, viral or fungal infections.
• Malignancy: increased risk of lymphomas and skin cancers with long‑term use.
• Severe allergic reactions: rash, angioedema, or anaphylaxis.

Before initiating therapy with ciclosporin, several precautionary measures should be observed to ensure patient safety.

• Renal function: monitor serum creatinine and glomerular filtration rate regularly.
• Blood pressure: check and control hypertension throughout treatment.
• Lipid profile: assess cholesterol and triglycerides before and during therapy.
• Infection risk: avoid use in patients with active uncontrolled infections.
• Pregnancy and lactation: evaluate risks versus benefits; use only if clearly needed.
• Store at ambient temperature: keep below 25 °C in the original container, protected from moisture and light.

Ciclosporin interacts with several medicines that can alter its plasma concentration or increase toxicity.

Major Interactions (Avoid)

• Ketoconazole, itraconazole, and other strong CYP3A4 inhibitors: can markedly raise ciclosporin levels, risking nephrotoxicity.
• Rifampicin and other CYP3A4 inducers: can substantially lower drug concentrations, reducing efficacy.
• St. John’s wort: herbal CYP3A4 inducer that may diminish immunosuppressive effect.

Moderate Interactions (Monitor Closely)

• NSAIDs and diuretics: may enhance renal toxicity when combined.
• Statins (especially simvastatin): increased risk of myopathy due to shared metabolism.
• Vaccines (live attenuated): potential for reduced vaccine efficacy or infection.